Granted Patent
B2
US 12,427,209 · App. 17/415,649 · Granted Sep 30, 2025
Dual mode 18F-labelled theranostic compounds and uses thereof
Inventors:
David Perrin (Vancouver, CA); Aron Roxin (Vancouver, CA); Mathieu Lepage (L'Huisserie, FR); Sungjoon Huh (Surrey, CA); Zhibo Liu (Beijing, CN); Rajaguru Kandasamy (Tamil Nadu, IN); Francois Benard (Vancouver, CA); Kuo-Shyan Lin (Richmond, CA); Hsiou-Ting Kuo (Vancouver, CA); Chengcheng Zhang (Richmond, CA)
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Abstract
A compound or molecular complex. The compound or molecular complex comprises: a metal chelator configured for chelation with a radioactive isotope or a non-radioactive isotope; and a trifluoroborate (BF 3 )-containing moiety configured for 19 F/ 18 F exchange or a precursor thereof; and optionally a cell-targeting domain.
Claims (13)
1. A compound or molecular complex comprising:
a metal chelator configured for chelation with a radioactive metal isotope or a non-radioactive metal isotope;
a cell-targeting domain; and
a trifluoroborate (BF 3 )-containing moiety configured for 19 F/ 18 F exchange or a boronate precursor that is capable of conversion to an 18 F-labeled trifluoroborate;
wherein the compound or molecular complex is selected from the group consisting of:
2. A method of imaging and treating a disease or condition in a subject, the method comprising:
(i) administering a compound or molecular complex according to claim 1 to the subject, wherein the BF 3 -containing moiety of the compound or molecular complex is labelled with 18 F, the metal chelator of the compound or molecular complex is chelated with a radioactive metal isotope or a non-radioactive metal isotope, and the cell targeting domain targets a cellular marker of the disease or condition, and imaging the subject to confirm the presence of the cellular marker; and
(ii) administering the compound or molecular complex to the subject, wherein the BF 3 -containing moiety is labeled with 19 F and/or 18 F, and the metal chelator is chelated with a therapeutic radioactive isotope.
3. A method of imaging and/or treating a disease or condition in a subject using a compound or molecular complex according to claim 1 in combination with a bispecific antibody, wherein the bispecific antibody is specific for both a cellular marker of the disease or condition and the metal chelator of the compound or molecular complex, the method comprising administering the bispecific antibody to the subject and one or both of the following steps:
(i) administering the compound or molecular complex to the subject wherein the BF 3 containing moiety of the compound or molecular complex is labelled with 18 F, wherein the metal chelator of the compound or molecular complex is chelated with a radioactive metal isotope or a non-radioactive metal isotope, and imaging the subject to confirm the presence of the cellular marker
(ii) administering the compound or molecular complex to the subject, wherein the BF 3 -containing moiety is labeled with 19 F and/or 18 F, and the metal chelator is chelated with a therapeutic radioactive isotope.
4. The method of claim 3 , wherein the compound or molecular complex is administered to the subject as a complex with the bispecific antibody.
5. The method of claim 3 , wherein the bispecific antibody is administered to the subject prior to administering the compound or molecular complex to the subject in a pre-targeting step during which the bispecific antibody binds to the cellular marker.
Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Mar 8, 2022
From: KUO, HSIOU-TING
To: THE UNIVERSITY OF BRITISH COLUMBIA
Reel/Frame 059196/0873 →
CORRECTIVE ASSIGNMENT TO CORRECT THE EXPUNGED 3RD ASSIGNOR'S NAME PREVIOUSLY RECORDED AT REEL: 056580 FRAME: 0242. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT .
Recorded Mar 8, 2022
From: BÉNARD, FRANÇOIS; LIN, KUO-SHYAN; ZHANG, CHENGCHENG
To: PROVINCIAL HEALTH SERVICES AUTHORITY
Reel/Frame 059349/0643 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Jun 17, 2021
From: BENARD, FRANCOIS; LIN, KUO-SHYAN; KUO, HSIOU-TING; ZHANG, CHENGCHENG
To: PROVINCIAL HEALTH SERVICES AUTHORITY
Reel/Frame 056580/0242 →
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Jun 17, 2021
From: PERRIN, DAVID; ROXIN, ARON; LEPAGE, MATHIEU; HUH, SUNGJOON; LIU, ZHIBO; KANDASAMY, RAJAGURU
To: THE UNIVERSITY OF BRITISH COLUMBIA
Reel/Frame 056580/0382 →
Continuity (2)
Provisional Application
62781584
· Dec 18, 2018
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